Authors: Ji Shan Quan, Hu Lin Jiang, Yun Jaie Choi, Mi Kyong Yoo, Chong Su Cho
Abstract: The aim of this study is to prepare mucoadhesive chitosan microspheres for protein drug
to deliver to intestine through oral administration. The thiolated Eudragit was synthesized by
reaction between L-cysteine hydrochloride and Eudragit® L-100. About 8 mol-% of cysteine was
introduced to the Eudragit-cysteine conjugate. The conjugate was used to coat bovine serum
albumin (BSA)-loaded chitosan microspheres. The average particle sizes of BSA-loaded thiolated
Eudragit-coated chitsoan microspheres (TECMs) were 4.06±0.74 .m and the uniform sizedistribution
was shown. The in vitro release of BSA from BSA-loaded TECMs was pH-dependent.
Our results indicated that thiolated Eudragit might be a good candidate as a coating material for oral
delivery of protein drug owing to mucoadhesive and pH-sensitive properties.
445
Authors: Ji Hye Seo, Hyun Seuk Moon, Ding Ding Guo, Hong Gu Lee, Yun Jaie Choi, Chong Su Cho
Abstract: The objective of this study is to investigate whether the PEGylated conjugated linoleic
acid (PCLA) as an anti-cancer prodrug can have favorable stability, biological activity, and
prevention of proliferation in MCF-7 breast cancer cells for anti-cancer when compared with
conjugated linoleic acid (CLA) itself. The CLA was simply coupled to poly(ethylene glycol) (PEG)
at melting state without solvent or catalyst through ester linkage between carboxylic group of CLA
and hydroxyl one of PEG. The results showed that the half life of PCLA was 55h in cell culture
medium at pH 7.4 and 37°C. Apoptosis of MCF-7 breast cancer cells were induced by not only
CLA- but PCLA-treatment with increasing concentrations whereas PCLA increased cell viability
when compared with CLA itself. These results indicate that the PCLA is a more stable and valuable
prodrug in that it has good stability and inhibition of cancer cell proliferation.
441
Authors: In Young Park, Tae Hee Kim, You Kyoung Kim, Yun Jaie Choi, Jae Woon Nah, Chong Su Cho
Abstract: The strategies developed for gene delivery are generally classified into two categories of
viral and non-viral vectors. The limitation of viral vectors, which have problems including toxicity,
immunogenicity and inflammatory response has led to the development of a novel, synthetic vectors
based on non-viral vectors. Chitosan, one of non-viral vectors, has been a good candidate in gene
delivery field. Moreover, galactosylated chitosan (GC) had the specific recognition of hepatocytes
by galactose in the GC. Also, carbonate apatite increased the rate of DNA endocytosis and the
efficiency of gene transfer. We describe here a new concept for improving cell specificity and
transfection efficiency by hybridization of carbonate apatite (CAp) with GC. The complex
formation was confirmed by agarose gel electrophoresis. The complex optimized through
controlling calcium ion and charge ratio was evaluated on the cell specificity and transfection
efficiency.
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Authors: Hu Lin Jiang, Rohidas B. Arote, Ji Shan Quan, Mi Kyong Yoo, You Kyoung Kim, In Yong Kim, Zhong Shan Hong, Hong Gu Lee, Xun Jin, Yun Jaie Choi, Chong Su Cho
Abstract: Thiolated polymers have been studied by many researchers because of the mucoadhesive
properties of thiol group. Alginate is a natural and biocompatible polymer that has been widely used
in drug delivery. In this study, thiolated chitosan microspheres (TCMs) were prepared by ionic
gelation process with tripolyphosphate and then, the bovine growth hormone (BGH) was loaded as
a model drug. Finally, the BGH-loaded TCMs (BTCMs) were coated with alginate to improve the
stability in gastrointestinal (GI) track. The alginate-coated BTCMs (ABTCMs) were observed as
spherical shapes. The average particle sizes of ABTCMs were 6.97±0.55 -m and the sizedistribution
was shown uniformly. Release of BGH from ABTCMs was decreased by coating with
alginate and increased rapidly with the change in medium pH from 1.2 to 7.4. Results indicate that
the ABTCMs have a potential as a drug carrier for oral drug delivery.
433
Authors: Ho Hyun Song, Mi Kyong Yoo, Hyun Seuk Moon, Yun Jaie Choi, Hyun Chul Lee, Chong Su Cho
Abstract: In this study, novel polycaprolactone/hydroxyapatite (PCL/HA) scaffolds were prepared to
increase mechanical properties and degradation of PCL/HA ones for bone tissue engineering. PCL
macromers were synthesized through the reaction of PCL diol (Mn: 530, 1250, and 2000) and PCL triol (Mn:
900) with acryloyl chloride and confirmed using nuclear magnetic resonance spectrometer (NMR) and
fourier transform infrared (FTIR). The PCL/HA scaffolds were prepared by cross-linking of PCL macromer
in the presence of HA by UV treatment and freeze drying methods. Mechanical property and porosity as well
as degradability of the PCL/HA scaffolds were also investigated. PCL/HA scaffolds showed faster
degradation and higher compressive modulus than those of PCL itself due to their low crystallinity and
modification of terminal groups. The pore morphology and pore sizes of the PCL/HA scaffold were checked
by scanning electron microscope (SEM). Cell cytotoxicity and proliferation of MG-63 osteoblast cultured
onto the PCL/HA scaffold was assessed by lactate dehydrogenase (LDH) assay and Alamar blue assay,
respectively. The novel PCL/HA scaffold appears to be suitable for bone substitutes.
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Authors: Hyun Seuk Moon, Hong Gu Lee, Ho Hyun Song, Yun Jaie Choi, Chong Su Cho
Abstract: The purpose of this study is to make use of trans10,cis12 CLA (t-CLA) that has potential
for proliferation and differentiation to form adipocyte on the collagen-coated surface. Results
provided evidences of good adhesion, growth, viability, and differentiation of adipocyte on
collagen-coated surface compared with non-coated surface. Also, the results showed that mouse
3T3-L1 preadipocyte can be successfully and reproducibly cultured on the collagen-coated surface,
and the adipocyte precursor cells placed on the collagen-coated surface are able to undergo full
maturation into adipocytes in the control cells. Moreover, glycerol-3-phosphate dehydrogenase
(GPDH) activity in 3T3-L1 preadipocyte cultured on collagen-coated surface with t-CLA was
higher than that on polystyrene (PS) surface due to higher cell adhesion and cell viability. These
results suggest that collagen coating may provide a promising approach to develop a new adipocyte
replacement strategy using CLA.
261
Authors: Tae Hee Kim, Jin Hua, Hyun Woo Kim, Myung Haing Cho, Jae Woon Nah, Yun Jaie Choi, Chong Su Cho
Abstract: The development of an efficient targeted gene delivery system into cells is an important
strategy for the advancement of gene therapy. The targeted gene delivery system is especially
important in non-viral gene transfer which shows the relative low transfection efficiency. And it also
opens the possibility of selective delivery of therapeutic plasmids to specific tissues. Chitosan has been
considered to be a good candidate for gene delivery system, since it is already known as a
biocompatible, biodegradable, and low toxic material with high cationic potential. However, low
specificity and low transfection efficiency of chitosan need to be overcome prior to clinical trial. In
this study, we focused on the chemical modification of chitosan for enhancement of cell specificity
and transfection efficiency.
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